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    • 2. 发明申请
    • TRYPTAMINE ANALOGUES AS 5-HT1-LIKE AGONISTS
    • 作为5-HT1型激动剂的三甲酚胺类似物
    • WO1994014771A1
    • 1994-07-07
    • PCT/EP1993003564
    • 1993-12-14
    • SMITHKLINE BEECHAM PLCPORTER, Roderick, AlanCOATES, William, John
    • SMITHKLINE BEECHAM PLC
    • C07D209/16
    • C07D401/04C07D209/14C07D209/16C07D401/14C07D403/04
    • A compound of structure (I), in which R is an optionally substituted 6- to 10-membered aryl or heteroaryl ring; suitably R is an optionally substituted 6- or 10-membered aryl ring such as phenyl or naphthyl; suitably R is an optionally substituted 6- to 10-membered heteroaryl ring containing from 1 to 4 nitrogen atoms. R is hydrogen, halogen, C1-4 alkyl, CN, NO2 or CF3; R is hydrogen, halogen, C1-4 alkyl, CN, NO2 or CF3; R is C(R )(R )CH2NR R , -CH = NNHC(NH)NH2 or a; R and R are independently hydrogen or C1-4 alkyl; R and R are the same or different and are each hydrogen or C1-4 alkyl or together with the nitrogen atom to which they are attached form a ring; R is hydrogen, C1-4 alkyl, or C3-6 alkenyl; R is hydrogen and R is hydrogen or hydroxy, or R and R together represent a bond; and q and m are independently 1 or 2; and pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds are 5-HT1-like agonists (or partial agonists) and as such are expected to have utility in medicine in the treatment and/or prophylaxis of migraine, and other conditions associated with cephalic pain, such as cluster headache, headache associated with vascular disorders and other neuralgia. They are also expected to have utility in the treatment or prophylaxis of portal hypertension.
    • 结构(I)的化合物,其中R 1是任选取代的6至10元芳基或杂芳基环; 合适的R 1是任选取代的6-或10-元芳环,例如苯基或萘基; 适当地,R 1是含有1至4个氮原子的任选取代的6至10元杂芳基环。 R 2是氢,卤素,C 1-4烷基,CN,NO 2或CF 3; R 3是氢,卤素,C 1-4烷基,CN,NO 2或CF 3; R 3是C(R 4)(R 5)CH 2 NR 6 R 7,-CH = NNHC(NH)NH 2或a; R 4和R 5独立地是氢或C 1-4烷基; R 6和R 7相同或不同,各自为氢或C 1-4烷基,或与它们所连接的氮原子一起形成环; R 8是氢,C 1-4烷基或C 3-6烯基; R a是氢,R b是氢或羟基,或R a和R b一起表示键; q和m独立地为1或2; 及其药学上可接受的盐,溶剂化物和水合物。 化合物是5-HT1样激动剂(或部分激动剂),因此预期在医学中可用于治疗和/或预防偏头痛以及与头痛相关的其它病症,例如丛集性头痛,与头痛相关的头痛 血管疾病等神经痛。 它们也预期可用于治疗或预防门静脉高压。